Eltrombopag

製品コードS4502 バッチS450202

印刷

化学情報

Chemical Structure Synonyms SB-497115 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H22N4O4
分子量 442.47 CAS No. 496775-61-2
Solubility (25°C)* 体外 DMSO 14 mg/mL warmed with 50ºC water bath (31.64 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Eltrombopag (SB-497115), a member of the biarylhydrazone class, is a nonpeptide agonist of the thrombopoietin receptor (TpoR), used to treat chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP).
in vitro Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. [3]
in vivo Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. [1] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [3]

プロトコル(参考用のみ)

カスタマーフィードバック

Data from [Data independently produced by , , J Cell Mol Med, 2018, 22(11):5367-5377]

Data from [Data independently produced by , , Int J Oncol, 2015, 47(5):1696-702.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Eltrombopag Preserves the Clonogenic Potential of Hematopoietic Stem Cells During Treatment With Antithymocyte Globulin in Patients With Aplastic Anemia [ Hemasphere, 2023, 7(6):e906] PubMed: 37304936
Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells [ Am J Cancer Res, 2022, 12(6):2697-2710] PubMed: 35812066
Iron Status Influences the Response of Cord Blood Megakaryocyte Progenitors to Eltrombopag in Vitro [ Blood Adv, 2021, bloodadvances.2021004207] PubMed: 34654056
Eltrombopag inhibits Type I interferon-mediated antiviral signaling by decreasing cellular iron [ Biochem Pharmacol, 2021, 186:114436] PubMed: 33539815
The Thrombopoietin Receptor Agonist Eltrombopag Inhibits Human Cytomegalovirus Replication Via Iron Chelation. [ Cells, 2019, 9(1)] PubMed: 31861948
The synergistic antileukemic effects of eltrombopag and decitabine in myeloid leukemia cells. [ Cancer Manag Res, 2019, 11:8229-8238] PubMed: 31564981
Repurposing the thrombopoietin receptor agonist eltrombopag as an anticryptococcal agent. [ Med Mycol, 2019, myz077] PubMed: 31297540
Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist [Xie C J Cell Mol Med, 2018, 22(11):5367-5377] PubMed: 30156363
Solitary Inhibition of the Breast Cancer Resistance Protein Efflux Transporter Results in a Clinically Significant Drug-Drug Interaction with Rosuvastatin by Causing up to a 2-Fold Increase in Statin Exposure [Elsby R Drug Metab Dispos, 2016, 44(3):398-408] PubMed: 26700956
Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure [Elsby R, et al. Drug Metab Dispos, 2015, 44(3):398-408] PubMed: 26700956

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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